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Assay Detail

CHEMBL4430338

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Functional
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel multifunctional dopamine D<sub>2</sub>/D<sub>3</sub> receptors agonists with potential neuroprotection and anti-alpha synuclein protein aggregation properties.
Luo D, Sharma H, Yedlapudi D, Antonio T, Reith MEA, Dutta AK.
Bioorg Med Chem (2016) 24 : 5088 -5102
PubMed 27591013 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 8.65 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4538230 1 9.48
CHEMBL4452046 1 9.11
CHEMBL4466245 1 8.91
CHEMBL4457171 1 8.58
CHEMBL59 DOPAMINE 4.0 1 8.14
CHEMBL4573578 1 7.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4538230 EC50 = 0.33 nM 9.48
CHEMBL4452046 EC50 = 0.78 nM 9.11
CHEMBL4466245 EC50 = 1.22 nM 8.91
CHEMBL4457171 EC50 = 2.62 nM 8.58
CHEMBL59 DOPAMINE EC50 = 7.26 nM 8.14
CHEMBL4573578 EC50 = 20.4 nM 7.69